114 results about "Azepindole" patented technology

This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.

The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with new piperidine 4-alkenyl derivatives that possess unique antiviral activity. More particularly, the present invention relates to compounds useful for the treatment of HIV and AIDS. The compounds of the invention for the general Formula I: wherein: Z is Q is selected from the group consisting of: -W- is

Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor a_2A. The compounds may also bind to and are an antagonist of the adrenergic receptor α_2B; or the compounds are not antagonists of the adrenergic receptor α2β and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.

Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor α_2A. The compounds may also bind to and are an antagonist of the adrenergic receptor α_2B; or the compounds are not antagonists of the adrenergic receptor α_2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.

The invention comprises substituted diazaindole-dicarbonyl-piperazinyl derivatives of general Formula I

wherein:

Q is selected from the group consisting of — may represent a bond; T is —C(O)— or —CH(CN)—; and

—Y— is selected from the group consisting of

compositions thereof and their use for treating HIV infection.

The present invention presents compounds that inhibit phosphodiesterase 4 having Formula (I). The present invention also provides methods of using the compounds of Formula (I) to prevent or treat asthma, atopic dermatitis, rheumatoid arthritis, inflammatory bowel disorders, pulmonary hypertension, liver injury, bone loss, septic shock, or multiple sclerosis, and to pharmaceutical compositions that contain the compounds of Formula (I).

A method for designing and synthesizing 7-azaindirubin and 7-azaisoindigo derivative and its medicinal use are disclosed. It changes indirubin and isoindigo nuclear-parent molecule atomic composition to form into compound. It also changes original molecule electric property. The process is carried out by coupling at different position by 7-azaindole and indole bi-molecule, inhibiting CDKs and CDKIs growth and breed and inducing CDKIs biological function. It can be used to treat malignant tumor, HIV and nervous system diseases.

This invention provides compounds of Formula I, including pharmaceutically accceptable salts thereof, having drug and bio-affecting properties, their pharmaceutical compositions and method of use. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. The compounds of Formula I have the formula

wherein:

Z is

Q is selected from the group consisting of

m is 2; A is selected from the group consisting of cinnolinyl, napthyridinyl, quinoxalinyl, pyridinyl, pyrimidinyl, quinolinyl, isoquinolinyl, quinazolinyl, azabenzofuryl, and phthalazinyl each of which may be optionally substituted with one or two groups independently selected from methyl, methoxy, hydroxy, amino and halogen; and

—W— is

The invention relates to azaindole derivatives, a preparation method and applications thereof in medicine. Specifically, the invention relates to novel derivatives represented by the formula (I), pharmaceutically acceptable salts thereof, pharmaceutical composition containing the derivatives, and a preparation method of the derivatives. The invention also discloses an application of the derivatives, pharmaceutically acceptable salts thereof, or pharmaceutical composition containing the derivative in the preparation of drugs for treating and/or preventing inflammation related diseases, especially Janus kinase 3 (JAK3) inhibitor. The definitions of each substituent in the formula (I) are the same as the definitions in the description.

The present invention relates to 2,3-Substituted Azaindole Derivatives, compositions comprising at least one 2,3 -Substituted Azaindole Derivatives, and methods of using the 2,3-Substituted Azaindole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.

A compound useful as an AMPK-activating agent is provided. A compound represented by formula (I) (wherein X represents a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, a substituted or unsubstituted cycloalkyl group, a substituted or unsubstituted cycloalkenyl group or a substituted or unsubstituted heterocyclyl group; R1 represents a hydrogen atom, a halogen atom, a cyano group, a nitro group, a carboxy group, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted acyl group, a substituted or unsubstituted carbamoyl group, a substituted or unsubstituted alkylthio group, a substituted or unsubstituted alkylsulfinyl group, a substituted or unsubstituted alkylsulfonyl group or a substituted or unsubstituted alkyloxycarbonyl group; R2 represents a halogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, a substituted or unsubstituted cycloalkyl group, a substituted or unsubstituted cycloalkenyl group, a substituted or unsubstituted heterocyclyl group or the like; R3 represents a halogen atom, a hydroxy group, a cyano group, a nitro group, a carboxy group, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, a substituted or unsubstituted cycloalkyl group, a substituted or unsubstituted cycloalkenyl group, a substituted or unsubstituted heterocyclyl group or the like; and R4 represents a hydrogen atom, a halogen atom, a hydroxy group, a cyano group, a nitro group, a carboxy group, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group or the like) or a pharmaceutically acceptable salt thereof.

The invention belongs to the field of medicine. In particular, the invention relates to a preparation method of a series of indole or azaindole derivatives and medicinal salt thereof, a medicinal composition containing the derivatives, and application of the derivatives and the medicinal composition to preparation of anti-gout medicines and treatment on related diseases. The structural formula ofthe compound is shown in the description.

The invention relates to azaindole with regioselectivity and a synthetic method thereof, and mainly solves the technical problems that no document reports the synthesis of azaindole with regioselectivity, and the structure-function relationship of the pharmaceutical activity of the azaindole is screened. The structure general formula is as follows (as shown in the specification), R1 and R2 are substituent groups on the pentabasic pyrrole ring of the azaindole, and can be hydrogen, straight chains, side chains or ring-shaped alkyl groups, R3 is an alkyl group on the hexahydric n-heterocyclic of the azaindole, a halogen substituent group or a hydrogen atom without substitution, and A is one of carbon atom or nitrogen heteroatom.

This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with ureido and thioureido piperazine derivatives of Formula I. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.

The compounds of Formula I are

wherein:

Y is O or S;

Q is selected from the group consisting of

m is 2;

• • A is NR¹³R¹⁴; and

—W— is

The invention relates to the field of organic synthesis and medicine, and discloses a preparation method for 4-substituted-7-azaindole. Firstly, N-oxide-7-azaindole is prepared by employing 7-azaindole as a raw material and hydrogen peroxide as an oxidizing agent; then 4-halogenated-7-azaindole is synthesized by adding acetonitrile and phosphorus oxyhalides (POX3) and by using diisopropyl ethyl amine as a catalyst; and 4-methoxy-7-azaindole is synthesized by reacting the synthesized 4-halogenated-7-azaindole and alkoxide. The 4-substituted-7-azaindole synthesized by the method has high yield and low cost, and the method is easy for industrialization.